Radiochemistry: a hot field with opportunities for cool chemistry

GD Bowden, PJH Scott, E Boros - ACS Central Science, 2023 - ACS Publications
Recent Food and Drug Administration (FDA) approval of diagnostic and therapeutic
radiopharmaceuticals and concurrent miniaturization of particle accelerators leading to …

Can Machine Learning Overcome the 95% Failure Rate and Reality that Only 30% of Approved Cancer Drugs Meaningfully Extend Patient Survival?

D Sun, C Macedonia, Z Chen… - Journal of Medicinal …, 2024 - ACS Publications
Despite implementing hundreds of strategies, cancer drug development suffers from a 95%
failure rate over 30 years, with only 30% of approved cancer drugs extending patient …

Strategies for designing novel positron emission tomography (PET) radiotracers to cross the blood–brain barrier

A Lindberg, M Chassé, C Varlow… - Journal of Labelled …, 2023 - Wiley Online Library
Positron emission tomography (PET) is a powerful tool for imaging biological processes in
the central nervous system (CNS). Designing PET radiotracers capable of crossing the …

[HTML][HTML] Design, synthesis and preclinical evaluation of muscarine receptor antagonists via a scaffold-hopping approach

M Millard, J Kilian, M Ozenil, M Mogeritsch… - European Journal of …, 2023 - Elsevier
Our research group recently identified a rearrangement product of pirenzepine as starting
point for a comprehensive rational drug design approach towards orthosteric muscarinic …

Ligand-Based Virtual Screening as a Path to New Chemotypes for Candidate PET Radioligands for Imaging Tauopathies

BT Hurtle, S Jana, L Cai, VW Pike - Journal of Medicinal …, 2024 - ACS Publications
Ligand-based virtual screening (LBVS) has rarely been tested as a method for discovering
new structural scaffolds for PET radioligand development. This study used LBVS to discover …

Identification of novel tau positron emission tomography tracers for chronic traumatic encephalopathy by comprehensive in silico screening and molecular dynamics …

B Qi, L Guan, J Tan, G Li, Y Sun, Q Zhang… - Physical Chemistry …, 2025 - pubs.rsc.org
Chronic traumatic encephalopathy (CTE), a neurodegenerative disease associated with
repetitive mild traumatic brain injury, is characterized neuropathologically by abnormal …

[HTML][HTML] Investigating experimental vs. Predicted pKa values for PET radiotracer

SL Stellnberger, R Harvey… - European Journal of …, 2024 - Elsevier
The prediction of central nervous system (CNS) active pharmaceuticals and
radiopharmaceuticals has experienced a boost by the introduction of computational …

PET Ligands for Imaging Mutant Huntingtin Aggregates: A Case Study in Non‐For‐Profit Scientific Management

CGF Dickmann, S Milicevic Sephton, RA Barker… - …, 2024 - Wiley Online Library
Positron emission tomography imaging of misfolded proteins with high‐affinity and selective
radioligands has played a vital role in expanding our knowledge of neurodegenerative …

Historical efforts to develop 99mTc-based amyloid plaque targeting radiotracers

G Takalloobanafshi, A Kukreja… - Frontiers in Nuclear …, 2022 - frontiersin.org
Imaging biomarkers have changed the way we study Alzheimer's disease and related
dementias, develop new therapeutics to treat the disease, and stratify patient populations in …

Proceedings of international symposium of trends in radiopharmaceuticals 2023 (ISTR-2023)

A Jalilian, C Decristoforo, M Denecke… - EJNMMI …, 2023 - Springer
Abstract The International Atomic Energy Agency (IAEA) held the 3rd International
Symposium on Trends in Radiopharmaceuticals,(ISTR-2023) at IAEA Headquarters in …